Assay Detail
Binding
CHEMBL2422303
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Inhibition of human recombinant TRPC6 expressed in HEK293-MSRII cells assessed as carbachol-stimulated Ca2+/Na+ influx after 10 mins by FLIPR assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293-MSRII |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Short transient receptor potential channel 6 (CHEMBL2417347) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The discovery of potent blockers of the canonical transient receptor channels, TRPC3 and TRPC6, based on an anilino-thiazole pharmacophore.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 6.52 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2418809 | — | — | 1 | 8.40 |
| CHEMBL2418807 | — | — | 1 | 7.80 |
| CHEMBL2418811 | — | — | 1 | 7.80 |
| CHEMBL2418808 | — | — | 1 | 7.60 |
| CHEMBL2418815 | — | — | 1 | 7.50 |
| CHEMBL2418810 | — | — | 1 | 7.30 |
| CHEMBL2418814 | — | — | 1 | 7.20 |
| CHEMBL2418806 | — | — | 1 | 7.10 |
| CHEMBL2418823 | — | — | 1 | 6.80 |
| CHEMBL2418813 | — | — | 1 | 6.80 |
| CHEMBL2418818 | — | — | 1 | 6.40 |
| CHEMBL1506485 | — | — | 1 | 6.30 |
| CHEMBL2418824 | — | — | 1 | 6.20 |
| CHEMBL2418822 | — | — | 1 | 6.20 |
| CHEMBL2418820 | — | — | 1 | 6.10 |
| CHEMBL2418819 | — | — | 1 | 6.10 |
| CHEMBL2418816 | — | — | 1 | 5.90 |
| CHEMBL2418812 | — | — | 1 | 5.80 |
| CHEMBL2418804 | — | — | 1 | 5.80 |
| CHEMBL2418821 | — | — | 1 | 5.50 |
| CHEMBL2418805 | — | — | 1 | 5.40 |
| CHEMBL2418817 | — | — | 1 | 5.20 |
| CHEMBL2418825 | — | — | 1 | 4.80 |
| CHEMBL2417565 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2418809 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2418807 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL2418811 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL2418808 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL2418815 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL2418810 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL2418814 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL2418806 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL2418823 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL2418813 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL2418818 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL1506485 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL2418824 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL2418822 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL2418820 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL2418819 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL2418816 | — | IC50 | = | 1260.0 | nM | 5.90 |
| CHEMBL2418812 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL2418804 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL2418821 | — | IC50 | = | 3160.0 | nM | 5.50 |
| CHEMBL2418805 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL2418817 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL2418825 | — | IC50 | = | 15800.0 | nM | 4.80 |
| CHEMBL2417565 | — | IC50 | > | 25000.0 | nM | - |